blu-701

BLU-701 is a novel, orally administered small molecule that acts as a highly selective fourth-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. It is designed to target tumors with EGFR exon 19 deletion or L858R point mutations and the C797S resistance mutation, which are common in non-small cell lung cancer (NSCLC). Unlike earlier EGFR inhibitors, BLU-701 spares wild-type EGFR and demonstrates nanomolar potency against both activating and resistance mutations. The drug is brain-penetrant and has shown preclinical antitumor activity in both treatment-naïve and osimertinib-resistant models of NSCLC, including central nervous system metastases. Developed by Blueprint Medicines, BLU-701 was investigated as monotherapy or in combination with other therapies such as osimertinib or platinum-based chemotherapy for patients with advanced EGFR-mutant NSCLC[1][2][3][6][7].